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- Title
Site-selective radiolabeling of peptides by F-fluorobenzoylation with [F]SFB in solution and on solid phase: a comparative study.
- Authors
Kuchar, Manuela; Pretze, Marc; Kniess, Torsten; Steinbach, Jörg; Pietzsch, Jens; Löser, Reik
- Abstract
Peptides labeled with short-lived positron-emitting radionuclides are of outstanding interest as probes for molecular imaging by positron emission tomography (PET). Herein, the site-selective incorporation of fluorine-18 into lysine-containing peptides using the prosthetic labeling agent N-succinimidyl 4-[F]fluorobenzoate ([F]SFB) is described. The reaction of [F]SFB with four biologically relevant resin-bound peptides was studied and optimized. For comparison, each peptide was F-fluorobenzoylated in solution under different conditions and the product distribution was analyzed confirming the advantages of the solid-phase approach. The method's feasibility for selective radiolabeling either at the N-terminus or at the lysine side chain was demonstrated. Labeling on solid phase with [F]SFB resulted in crude F-fluorobenzoylpeptides whose radiochemical purities were typically greater than 90% and that could be prepared in synthesis times from 65 to 76 min.
- Subjects
SOLID-phase synthesis; RADIOLABELING; COMPARATIVE studies; SOLUTION (Chemistry); FLUORINE; POSITRON emission tomography; BENZOATES
- Publication
Amino Acids, 2012, Vol 43, Issue 4, p1431
- ISSN
0939-4451
- Publication type
Article
- DOI
10.1007/s00726-012-1216-z